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Flashcards in Neuro Pharm Deck (95)
1

Glaucoma drugs: classes and specific drugs

1. alpha agonists: epinephrine, brimonidine
2. beta blockers: timolol, betaxolol, careolol
3. diuretics: acetazolamide
4. cholinomimetics:
direct: carbachol, pilocarpine
indirect: physostigmine, echothiophate
5. prostaglandin: latanoprost

2

Glaucoma - Epinephrine

1. mechanism
2. side effects
3. c/i

1. alpha agonist: decrease aq humour synthesis through vasoconstriction
2. mydriasis, stinging
3. DO NOT USE in closed angle glaucoma

3

Glaucoma - Brimonidine

1. mechanism
2. side effects

1. alpha 2-agonist, decreases aq humor synthesis
2. none

4

Glaucoma - Beta blockers

1. mechanism
2. side effects

1. decrease aq humour secretion
2. none

timilol, betaxolol, carteolol

5

Glaucoma - Acetazolamide

1. mechanism
2. side effects

1. decrease aq humour secretion by decreasing HCO3- via inhibition of carbonic anhydrase
2. none

6

Glaucoma - Cholinomimetics

1. mechanism
2. side effects

1. Increase outflow of aq humour, contract ciliary muscle (which produces aq humour) and opens trabecular network into canal of Schlemm
2. miosis, cyclospasm (accomodate)

7

Which glaucoma drug do you use in an emergency?

Pilocarpine

8

Glaucoma - Latanoprost

1. mechanism
2. side effects

1. Prostaglandin (PGFa2), increase outflow of aq humour
2. Darkens iris (browning)

9

Opioid analgesics - drugs

Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan

10

Opioid analgesics - mechanism

Agonist at opioid receptors, mu (morphine), delta (enkephalin), kappa (dynorphin)

Open K close Ca channels --> decrease synaptic transmission

Inhibit release of ACh, NE, 5HT, glutamate, substance P

11

Opioid analgesics - use

Pain
Cough suppression (dextromethorphan)
Diarrhea (loperamide and diphenoxylate)
Acute pulmonary edema
Maintenance program for addicts (methadone)

12

Which opioid is used for cough suppression?

Dextromethorphan

13

Which opioids are used for diarrhea?

Loperamide and diphenoxylate

14

Which opioids are used for maintenance in drug addicts?

Methadone

15

Toxicity of opioid analgesics

Tolerance
Respiratory depression
Constipation
Miosis
CNS depression with other drugs

16

What do you treat opioid toxicity with?

Opioid receptor antagonists:
naltrexone
naloxone

17

What do you NOT develop tolerance to when using opioids?

Miosis
Constipation

18

Butorphanol

Mechanism
Use
Toxicity

1. Partial agonist at opioid mu receptors, agonist at kappa
2. Pain, causes less respiratory depression than full agonists
3. Causes withdrawal if on full agonists

19

Which opioid causes less respiratory depression in comparison to other opioids?

Butorphanol

20

Tramadol

1. Mechanism
2. Use
3. Toxicity

1. Weak opioid agonist, inhibits Serotonin and NE reuptake (works on multiple neurotransmitters)

2. chronic pain

3. decreases seizure threshold

21

Phenytoin

1. Tx's which seizures
2. Mechanism
3. Which drug can be used parenterally?

1. Simple Partial
Simple Complex
1st line for Generalized Tonic-Clonic
1st line for Status

2. Use dependent blockade of Na+ channels, decrease refractory period, inhibit glutamate release form excitatory presynaptic neurons

3. Fosphenytoin

22

Phenytoin toxicity

Gingival hyperplasia in kids
Hirsutism
Megaloblastic anemia (decreases folate absorption)
Teratogenesis (fetal hydantoin syndrome)
SLE-like syndrome
Cyt-P450 inducer
SJS

23

Carbamezapine

1. Tx's which seizures
2. Mechanism
3. SE

1st line for all Simple Partial, Simple Complex, Generalized Tonic-Clonic

2. Increases Na channel inactivation
3. diplopia, ataxia, blood dyscrasias, liver tox, teratogenesis, cP450 inducer, SIADH, SJS

24

Which drug is 1st line for trigeminal neuralgia?

Carbamezapine

25

Lamotrigine

1. Tx's which seizures
2. Mechanism
3. SE

1. PS, PC, GTC

2. Blocks voltage-gated Na channels
3. SJS

26

Gabapentin

1. Tx's which seizures
2. Mechanism
3. SE
4. other uses

1. PS, PC, GTC

2. GABA analogue, blocks high voltage activated Ca channels
3. Sedation, ataxia
4. peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder

27

Topiramate

1. Tx's which seizures
2. Mechanism
3. SE
4. other uses

1. PS, PC, GTC

2. Blocks Na channels, increases GABA action
3. sedation, metal dulling, kidney stones, weight loss
4. migraine preention

28

Phenobarbital

1. Tx's which seizures
2. Mechanism
3. SE

1. PS, PC, GTC

2. Increases duration of Cl- channel opening, increases GABA action
3. sedation, tolerance, dependence, cP450 inducer

29

Which AED is the first line for kids and pregnant women?

Phenobarbital

30

Which drugs are first line for GTC seizures?

Phenytoin
Carbamezapine
Valproic acid

31

Valproic acid

1. Tx's which seizures
2. Mechanism
3. SE
4. other uses

1. PS, PC, 1st line for GTC

2. Increase Na inactivation, increase GABA action via GABA transaminase inhibition
3. GI distress, hepatotoxicity, neural tube defects, tremor, weight gain
4. myoclonic seizures, bipolar disorder

32

Which AED is also used for myoclonic seizures?

Valproic acid

33

Ethosuximide

1. Tx's which seizures
2. Mechanism
3. SE

1. 1st line for absence seizures

2. Block Ca channels in thalamus
3. fatigue, GI distress, headact, itching, SJS, urticaria

34

Benzo's

1. Tx's which seizures
2. Mechanism

1. first line for acute status epilepticus

2. increase frequency of Cl- channel opening

35

Tiagabine

1. Tx's which seizures
2. Mechanism

1. PS, PC

2. inhibit GABA reuptake

36

Vigabatrin

1. Tx's which seizures
2. Mechanism

1. PS, PC

2. inhibits GABA transaminase, increasing GABA

37

Levetiracetam

1. Tx's which seizures
2. Mechanism

1. PS, PC, GTC

2. Unknown

38

Which AEDs are first line for status epilepticus?

Prophylaxis: Phenytoin

Acute: Benzo

39

Which AED is used for seizures in eclampsia?

Benzo

MgSO4 is first line

40

What are the only drugs for absence seizures?

ethosuximide is first line for absence and is only used for that
valproic acid can be used

41

Most of the seizure drugs are associated with what classes?

simple, complex, tonic-clonic

42

Benzodiazepine toxicities

Sedation
Tolerance
Dependance

43

Stevens-Johnsons syndrome

Sx's
AEDs that have this SE

1. Prodrome of malaise and fever

Rapid onset erythematous/purpuric macules (oral, ocular, genital)

Epidermal necrosis and sloughing

2. Ethosuximide
Carbamezapine
Lamotrigine
Phenytoin

44

Phenytoin is also what type of drug in addition to being an AED?

Class I antiarrhythmic

45

Barbiturates:

1. Examples of drugs
2. Use
3. Toxicites
4. Tx overdose?

1. Phenobarbital, pentobarbital, Thiopental
, secobarbital
2. Anxiety, seizures, insomnia, induction for anesthesia
3. additive CNS depression
respiratory/CV depression
induction of Cyt-P450
4. symptom management -- assist respiration and increase BP

46

Which AED is contraindicated in porphyria?

Barbiturates

47

Benzodiazepines

1. use
2. list short-acting drugs
3. toxicity

1. anxiety, spasticity, epilepticus, detox from EtOH, night terrors, sleep walking, general anesthetic, hypnotic

2.
Triazolam
Oxazepam
Midazolam

3. dependance
additive CNS depression with EtOH
less risk of respiratory depression and coma

48

How do you Tx benzo overdose?

Flumazenil

GABA receptor antagonist

49

Which benzo's have the highest addictive potential?

Short acting

Triazolam
Oxazepam
Midazolam

50

Which 2 AEDs are used for acute status epileptices?

Diazepam
Lorazepam

(Benzo's)

51

How do CNS drugs cross BBB?

1. soluble in lipid

OR

2. transporter

52

Drugs with decreased solubility in the blood have:

rapid induction and recovery times

53

Drugs with increased solubility in lipids have:

Increased potency

54

Potency of anesthetic drug =

1/MAC

MAC = minimal alveolar concentration

55

What does a large MAC mean in terms of potency?

low potency

56

MAC

minimal alveolar concentration at which 50% of population is anesthetized

57

how do barbiturates and benzos effect the GABA receptor?

barbiturates increase the duration of the Cl- channel opening while benzos increase the frequency

58

1. What are the nonbenzodiazepine hypnotics?
2. MOA
3. clinical use
4. toxicity

1. zolpidem, zaleplon, eszopliclone
2. BZ1 subtype of GABAR, reversed with flumazenil
3. insomnia
4. ataxia, heaches, confusion

59

Halothane has increased blood and lipid solubility, what does this mean in terms of potency and induction?

increased blood solubility: slow induction

increased lipid solubility: high potency

60

Mechanism of anesthetic action in lungs

increases rate and depth of ventilation

61

Mechanism of anesthetic action in blood

increased blood solubility: increase gas required to saturate blood --> slow induction time

62

Mechanism of anesthetic action in tissue (i.e. brain)

increased solubility: increased gas required to saturate tissue --> slower onset of action

63

Inhaled anesthetics

1. Drug examples
2. Mechanism
3. Effects
4. Toxicity

1. Halothane, isoflurane, nitrous oxide

2. unknown

3. myocardial and respiratory depression
nausea/emesis
increased cerebral blood flow (decreased cerebral metabolic demand)

4. Hepatotoxicity - halothane
Nephrotoxicity - methoxyflurane
Proconvulsant - enflurane
Malignant hyperthermia

64

How do you treat malignant hyperthermia?

dantrolene

65

IV anesthetics (5)

Barbiturates
Benzodiazepine
Ketamine
Opiates
Propofol

66

Thiopental

1. Potency, lipid solubility, entry time into brain
2. use
3. effect terminated by
4. effect on cerebral blood flow

IV anesthetic, barbiturate

1. high potency, high lipid solubility, rapid entry

2. induction anesthesia, short surgical procedures

3. redistribution into fat and tissues

4. decreases cerebral blood flow

67

Benzo's

1. use in anesthesia
2. used in conjuction with
3. toxicity

1. IV anesthetic, midazolam most commonly used for endoscopy
2. gas anesthetics and narcotics
3. severe post-op respiratory depression, amnesia

68

Ketamine
(arylcyclohexamine)

1. analog of
2. blocks which receptors
3. simulates
4. side effects

1. PCP, dissociative anesthesia
2. NMDA
3. CV system
4. disorientation, hallucination, bad dreams, increases cerebral blood flow

69

Opiates used as IV anesthetics

Morphine, fentanyl

70

Propofol

1. use
2. mechanism

1. IV rapid induction of anesthesia, short procedures

2. potentiates GABA
-A

Less post-op nausea than thiopental

71

Ester local anesthetics

Procaine, cocaine, tetracaine

72

Amide local anesthetics

lidocaine, mepivacaine, bupivacaine

(amides have 2 i's each)

73

Local anesthetics: mechanism

block Na channels

binds better to activated Na channels, so most effective in rapidly firing neurons

74

Tertiary local amides penetrate membrane in what form and bind to ion channels in what form?

penetrate in uncharged
bind in charged form

75

In infected (acidic) tissue, how must local anesthetics be administered differently?

Alkaline anesthetics are charged and can't penetrate acidic membrane effectively, so must administer more

76

Order of nerve blockade in local anesthetics

small fibers > large fibers

myelinated fibers > unmyelinated

Size factor predominates over myelination.

77

Order of sensory loss in local anesthetics

Pain>temperature>touch>pressure

78

Local anesthetics are usually given with what drug and why?

Vasoconstrictors (epi), they enhance local action

*except cocaine

79

Local anesthesia toxicity

CNS excitation
Severe CV toxicity (bupivacaine)
HTN
Hypotension
Arrhythmias (cocaine)

80

NMJ blockers

1. use
2. selective for which receptor
3. types

1. muscle paralysis in surgery or mechanical ventilation
3. Motor nicotinic
3. Depol and Non-depol

81

Succinylcholine

1. class
2. reversal of blockade
3. complications

1. cholinomimetic, NMJ depolarizing blocker

2. Phase 1: prolonged depol, no antidote
, potentiated by cholinesterase inhibitors
Phase 2: repolarized but blocked, can reverse with AChE inhibitors (neostigmine)
3. Hypercalemia, Hyperkalemia, malignant hyperthermia

82

Non-depolarizing NMJ blockers

1. examples
2. mechanism
3. reversal of blockade

1. tubocurarine, atracurium, pancuronium, etc.

2. competitive antagonists for ACh

3. AChE inhibitors (neostigime, edrophonium, etc.)

83

Dantrolene: use and mechanism

tx for malignant hyperthermia and neuroleptic malignant syndrome

prevents release of Ca from sarcoplasmic reticulum of skeletal muscle

84

Malignant hyperthermia is caused by

concomitant use of inhalational anesthetics (except N2O) and succinylcholine

85

Parkinson's has excess____ activity

cholinergic due to loss of dopaminergic neurons

86

PD drug classes

1. dopamine agonists - Bromocriptine

2. drugs that increase dopamine - Amantadine, L-dopa/carbidopa

3. prevent dopamine breakdown - Selegiline

4. decrease cholinergic activity - Benztropine

87

Dopamine agonists in PD:

examples
side effects

1. Bromocriptine (ergot), pramipexole, ropinorole (non-ergot, preferred)

2. gambling

88

Amantadine in PD

Increases dopamine release

also used as antiviral against influenza A

toxicity: ataxia

89

Selegiline

1. MOA
2. examples
3. adjunctive to what PD drug
4. toxicity

1. selective MAO-B inhibitor, which prefers metabolism of dopamine instead of NE or 5-HT

2. Entacapone, tocapone (COMT inhibitors)

3. L-dopa

4. enhance adverse effects of L-dopa

90

Benztropine in PD: MOA

anti-muscarinic (decreased cholinergic activity), improves tremor and rigidity, but little effect on bradykinesia

Park your Benz""

91

L-Dopa/carbidopa toxicity

arrhythmias from peripheral conversion of L-dopa

Long-term: dyskinesia after administration
Short-term: akinesia b/w doeses

92

Why is carbidopa given in PD?

peripheral decarboxylase inhibitor

decreases peripheral side effects of L-dopa and increases bioavailability in brain

93

AD Drugs (2)

1. MOA
2. toxicity

Memantine
1. NMDA receptor antagonist, helps prevent excitotoxicity mediated by Ca
2. dizziness, confusion, hallucinations

Donezapil, galantamine, rivastigmine
1. AChE inihibitor
2. Nausea, dizziness insomnia

94

Huntington's Drugs

1. alterations in NTs
2. drug classes and examples

1. Increased dopamine, decreased GABA and ACh

2. Reserpine + tetrabenzine - amine depleting
Haloperidol - dopamine receptor antagonist

95

Sumatriptan

1. MOA
2. Half-life
3. Use
4. Toxicity
5. c/i in

1. 5-HT agonist. Causes vasoconstriction, inhibits trigeminal activation and vasoactive peptide release.

2. s angina